Assay of Secoverine and Active Metabolites: Comparison of Stable Isotope Dilution with Receptor Binding Assay
Secoverine (formula below) is a new gastro-intestinal muscle relaxant whose pharmacokinetics and disposition are currently being investigated in different animal species and man. The drug is administered as a racemate of which only the (+) enantiomer has pharmacological activity. Human pharmacology revealed activity after either oral or parenteral administration. Plasma levels of the parent drug were hardly measurable (<1 ng/ml) after oral administration, whereas a similar i.v. dose resulted in plasma levels of ~10 ng/ml. Accordingly we investigated the occurrence of active metabolites. As urinary metabolite profiles did not provide any clue in this respect, we started in vitro experiments with 14C-labelled secoverine.
KeywordsHeptane Seco Trimethyl Rine Mandel
Unable to display preview. Download preview PDF.
- 1.Mazel, P. (1972) in Fundamentals of Drug Metabolism and Drug Disposition(La Du, B.N., Mandel, H.G. & Way, E.L., eds.), Williams & Wilkins, Baltimore, pp. 527 – 536.Google Scholar
- 2.Ruijten, H.M., de Bree, H., Borst, A.J.M., de Lange, N., Scherpenisse, P.M., Vincent, W.R. & Post, L.C. (1984) Drug Metab. Disp. 12, 82 – 92.Google Scholar